WO2000040569A8 - 2-oxy-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite - Google Patents

2-oxy-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite

Info

Publication number
WO2000040569A8
WO2000040569A8 PCT/GB2000/000031 GB0000031W WO0040569A8 WO 2000040569 A8 WO2000040569 A8 WO 2000040569A8 GB 0000031 W GB0000031 W GB 0000031W WO 0040569 A8 WO0040569 A8 WO 0040569A8
Authority
WO
WIPO (PCT)
Prior art keywords
reduced
formula
obesity
treatment
inhibition
Prior art date
Application number
PCT/GB2000/000031
Other languages
English (en)
Other versions
WO2000040569A1 (fr
WO2000040569A9 (fr
Inventor
Harold Francis Hodson
Robert Downham
Timothy John Mitchell
Beverley Jane Carr
Christopher Robert Dunk
Richard Michael John Palmer
Original Assignee
Alizyme Therapeutics Ltd
Harold Francis Hodson
Robert Downham
Timothy John Mitchell
Beverley Jane Carr
Christopher Robert Dunk
Richard Michael John Palmer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to JP2000592277A priority Critical patent/JP2002534419A/ja
Priority to DK00900081T priority patent/DK1144395T3/da
Application filed by Alizyme Therapeutics Ltd, Harold Francis Hodson, Robert Downham, Timothy John Mitchell, Beverley Jane Carr, Christopher Robert Dunk, Richard Michael John Palmer filed Critical Alizyme Therapeutics Ltd
Priority to CA002359987A priority patent/CA2359987C/fr
Priority to AT00900081T priority patent/ATE293610T1/de
Priority to SI200030674T priority patent/SI1144395T1/xx
Priority to HU0104909A priority patent/HUP0104909A3/hu
Priority to EP00900081A priority patent/EP1144395B1/fr
Priority to DE60019556T priority patent/DE60019556T2/de
Priority to AU18845/00A priority patent/AU770342B2/en
Priority to PL00350412A priority patent/PL350412A1/xx
Priority to NZ512739A priority patent/NZ512739A/en
Publication of WO2000040569A1 publication Critical patent/WO2000040569A1/fr
Publication of WO2000040569A8 publication Critical patent/WO2000040569A8/fr
Priority to NO20013380A priority patent/NO321058B1/no
Priority to US09/901,868 priority patent/US6656934B2/en
Publication of WO2000040569A9 publication Critical patent/WO2000040569A9/fr
Priority to US10/306,375 priority patent/US7776853B2/en
Priority to HK02109007.0A priority patent/HK1047284A1/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/041,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/121,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/141,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/241,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
    • C07D265/26Two oxygen atoms, e.g. isatoic anhydride
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/40Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
    • C07C271/58Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

L'invention concerne l'utilisation d'un composé de formule (I) ou d'un sel, d'un ester, d'un amide ou d'un promédicament dudit composé, pour inhiber une enzyme dont le mode d'action préféré est de catalyser l'hydrolyse d'une fonctionnalité ester, par exemple pour la régulation et l'inhibition des enzymes indésirables dans les produits et les processus. Ces composés sont également utiles en médecine, par exemple pour le traitement de l'obésité et des pathologies voisines. L'invention concerne également des composés de formule (I), des procédés permettant de les préparer et des compositions pharmaceutiques les contenant. Dans la formule (I), A est un noyau aromatique ou hétéro-aromatique à 6 éléments; et R1 est alkyle ramifié ou non ramifié (éventuellement interrompu par un ou plusieurs atomes d'oxygène), alcényle, alcinyle, cycloalkyle, cycloalcényle, aryle, arylalkyle, arylalkyle réduit, arylalcényle, hétéroaryle, hétéro-arylalkyle, hétéro-arylalcényle, aryle réduit, hétéro-aryle réduit, hétéro-arylalkyle réduit, ou un dérivé substitué de l'un des groupes ci-dessus.
PCT/GB2000/000031 1999-01-08 2000-01-06 2-oxy-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite WO2000040569A1 (fr)

Priority Applications (15)

Application Number Priority Date Filing Date Title
EP00900081A EP1144395B1 (fr) 1999-01-08 2000-01-06 2-amino-benzoxazinones destinees au traitement de l'obesite
DE60019556T DE60019556T2 (de) 1999-01-08 2000-01-06 2-amino-benzoxazinonderivate zur behandlung von fettleibigkeit
CA002359987A CA2359987C (fr) 1999-01-08 2000-01-06 2-oxy-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite
AT00900081T ATE293610T1 (de) 1999-01-08 2000-01-06 2-amino-benzoxazinonderivate zur behandlung von fettleibigkeit
SI200030674T SI1144395T1 (fr) 1999-01-08 2000-01-06
HU0104909A HUP0104909A3 (en) 1999-01-08 2000-01-06 2-amino-benzoxazinone derivatives for the treatment of obesity, process for their preparation and medicaments containing them
DK00900081T DK1144395T3 (da) 1999-01-08 2000-01-06 2-amino-benzoxazinon-derivater til behandling af fedme
JP2000592277A JP2002534419A (ja) 1999-01-08 2000-01-06 肥満治療用2−アミノ−4h−3,1−ベンゾオキサジン−4−オン誘導体
AU18845/00A AU770342B2 (en) 1999-01-08 2000-01-06 2-amino-4H-3,1-Benzoxazin-4-one derivatives for the treatment of obesity
NZ512739A NZ512739A (en) 1999-01-08 2000-01-06 2-amino-benzoxazinone derivatives for the treatment of obesity
PL00350412A PL350412A1 (en) 1999-01-08 2000-01-06 2−amino−benzoxazinone derivatives for the treatment of obesity
US09/901,868 US6656934B2 (en) 1999-01-08 2001-07-06 2-amino-benzoxazinone derivatives for the treatment of obesity
NO20013380A NO321058B1 (no) 1999-01-08 2001-07-06 Anvendelse av 2-aminobenzoksazinonderivater ved fremstilling av et medikament for profylakse eller behandling av overvekt eller en overvektsrelatert forstyrrelse, 2-aminobenzoksazinonderivater, fremgangsmate for fremstilling derav, farmasoytiske preparater og matprodukter som inneholder derivatene, anvendelser av derivatene samt kosmetisk fremgangsmate ved administrering derav.
US10/306,375 US7776853B2 (en) 1999-01-08 2002-11-27 2-amino-benzoxazinone derivatives for the treatment of obesity
HK02109007.0A HK1047284A1 (en) 1999-01-08 2002-12-12 2-amino-benzoxazinone derivatives for the treatment of obesity

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9900416.0A GB9900416D0 (en) 1999-01-08 1999-01-08 Inhibitors
GB9900416.0 1999-01-08

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US09/901,868 Continuation US6656934B2 (en) 1999-01-08 2001-07-06 2-amino-benzoxazinone derivatives for the treatment of obesity

Publications (3)

Publication Number Publication Date
WO2000040569A1 WO2000040569A1 (fr) 2000-07-13
WO2000040569A8 true WO2000040569A8 (fr) 2001-03-15
WO2000040569A9 WO2000040569A9 (fr) 2002-02-28

Family

ID=10845777

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2000/000031 WO2000040569A1 (fr) 1999-01-08 2000-01-06 2-oxy-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite

Country Status (22)

Country Link
US (2) US6656934B2 (fr)
EP (1) EP1144395B1 (fr)
JP (1) JP2002534419A (fr)
KR (1) KR100615914B1 (fr)
CN (1) CN100480245C (fr)
AR (1) AR022203A1 (fr)
AT (1) ATE293610T1 (fr)
AU (1) AU770342B2 (fr)
CA (1) CA2359987C (fr)
DE (1) DE60019556T2 (fr)
DK (1) DK1144395T3 (fr)
ES (1) ES2240051T3 (fr)
GB (1) GB9900416D0 (fr)
HK (1) HK1047284A1 (fr)
HU (1) HUP0104909A3 (fr)
MY (1) MY129247A (fr)
NO (1) NO321058B1 (fr)
NZ (1) NZ512739A (fr)
PL (1) PL350412A1 (fr)
PT (1) PT1144395E (fr)
RU (1) RU2244711C2 (fr)
WO (1) WO2000040569A1 (fr)

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9900416D0 (en) * 1999-01-08 1999-02-24 Alizyme Therapeutics Ltd Inhibitors
CA2286451A1 (fr) * 1999-10-14 2001-04-14 Grant A. Mitchell Induction de l'infertilite chez les males au moyen d'une lipase hormonosensible
GB0001572D0 (en) 2000-01-24 2000-03-15 Alizyme Therapeutics Ltd Inhibitors
EP1296656B1 (fr) 2000-06-27 2006-08-02 F. Hoffmann-La Roche Ag Procede de preparation de composition
ATE293477T1 (de) 2000-07-28 2005-05-15 Hoffmann La Roche Neue verwendung von lipase-inhibitoren
AU8969901A (en) 2000-07-28 2002-02-13 Hoffmann La Roche New pharmaceutical composition
US20030027786A1 (en) 2001-06-06 2003-02-06 Karsten Maeder Lipase inhibiting composition
US6730319B2 (en) 2001-06-06 2004-05-04 Hoffmann-La Roche Inc. Pharmaceutical compositions having depressed melting points
DE10135027A1 (de) * 2001-07-18 2003-02-06 Solvay Pharm Gmbh Verwendung Trifluoracetylalkyl-substituierter Phenyl-, Phenol- und Benzoylderivate in der Behandlung und/oder Prophylaxe von Obestias und deren Begleit- und/oder Folgeerkrankungen
US6943001B2 (en) 2001-08-03 2005-09-13 Diversa Corporation Epoxide hydrolases, nucleic acids encoding them and methods for making and using them
EP1578987A2 (fr) 2001-08-03 2005-09-28 Diversa Corporation Epoxyde-hydrolases, acides nucleiques codant ces hydrolases et procedes de fabrication et d'utilisation de celles-ci
CA2457976A1 (fr) 2001-08-22 2003-03-06 Aventis Pharma Deutschland Gmbh Preparations combinees contenant des derives de 1,4-benzothiepine-1,1-dioxyde ainsi que d'autres substances actives et utilisation desdites preparations
EP1446125B1 (fr) * 2001-08-30 2009-04-29 Alizyme Therapeutics Limited Thieno-(1,3)-oxazin-4-ones avec une activite inhibitrice des lipases
US7399777B2 (en) 2001-08-31 2008-07-15 Sanofi-Aventis Deutschland Gmbh Diarylcycloalkyl derivatives, processes for their preparation and their use as pharmceuticals
NZ531440A (en) 2001-08-31 2005-10-28 Aventis Pharma Gmbh Diaryl cycloalkyl derivatives, method for producing the same and the use thereof as PPAR activators
US6884812B2 (en) 2001-08-31 2005-04-26 Aventis Pharma Deutschland Gmbh Diarylcycloalkyl derivatives, processes for their preparation and their use as pharmaceuticals
KR20040068316A (ko) * 2001-12-20 2004-07-30 오에스아이 파마슈티컬스, 인코포레이티드 판크레아 리파제 저해제 화합물, 그의 합성방법 및사용방법
US7223796B2 (en) 2002-04-11 2007-05-29 Sanofi-Aventis Deutschland Gmbh Acyl-4-carboxyphenylurea derivatives, processes for preparing them and their use
US7078404B2 (en) 2002-04-11 2006-07-18 Sanofi-Aventis Deutschland Gmbh Acyl-3-carboxyphenylurea derivatives, processes for preparing them and their use
US7049341B2 (en) 2002-06-07 2006-05-23 Aventis Pharma Deutschland Gmbh N-benzoylureidocinnamic acid derivatives, processes for preparing them and their use
DE10231370B4 (de) 2002-07-11 2006-04-06 Sanofi-Aventis Deutschland Gmbh Thiophenglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
US7262220B2 (en) 2002-07-11 2007-08-28 Sanofi-Aventis Deutschland Gmbh Urea- and urethane-substituted acylureas, process for their preparation and their use
AU2003249937A1 (en) 2002-07-12 2004-02-02 Sanofi-Aventis Deutschland Gmbh Heterocyclically substituted benzoylureas, method for their production and their use as medicaments
US20040157922A1 (en) 2002-10-04 2004-08-12 Aventis Pharma Deutschland Gmbh Carboxyalkoxy-substituted acyl-carboxyphenylurea derivatives and their use as medicaments
US7208504B2 (en) 2002-10-12 2007-04-24 Sanofi-Aventis Deutschland Gmbh Bicyclic inhibitors of hormone sensitive lipase
DE10258007B4 (de) 2002-12-12 2006-02-09 Sanofi-Aventis Deutschland Gmbh Aromatische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel
US8372430B2 (en) 2002-12-17 2013-02-12 The Procter & Gamble Company Compositions, methods, and kits useful for the alleviation of gastrointestinal effects
US20040242583A1 (en) 2003-01-20 2004-12-02 Aventis Pharma Deutschland Gmbh Pyrimido[5,4-e][1,2,4]triazine-5,7-diones, processes for preparing them and their use
US7179941B2 (en) 2003-01-23 2007-02-20 Sanofi-Aventis Deutschland Gmbh Carbonylamino-substituted acyl phenyl urea derivatives, process for their preparation and their use
DE10306250A1 (de) 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7196114B2 (en) 2003-02-17 2007-03-27 Sanofi-Aventis Deutschland Gmbh Substituted 3-(benzoylureido) thiophene derivatives, processes for preparing them and their use
DE10308355A1 (de) 2003-02-27 2004-12-23 Aventis Pharma Deutschland Gmbh Aryl-cycloalkyl substituierte Alkansäurederivate, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel
US7148246B2 (en) 2003-02-27 2006-12-12 Sanofi-Aventis Deutschland Gmbh Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals
DE10308351A1 (de) 2003-02-27 2004-11-25 Aventis Pharma Deutschland Gmbh 1,3-substituierte Cycloalkylderivate mit sauren, meist heterocyclischen Gruppen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
DE10308352A1 (de) 2003-02-27 2004-09-09 Aventis Pharma Deutschland Gmbh Arylcycloalkylderivate mit verzweigten Seitenketten, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel
DE10308353A1 (de) 2003-02-27 2004-12-02 Aventis Pharma Deutschland Gmbh Diarylcycloalkylderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7501440B2 (en) 2003-03-07 2009-03-10 Sanofi-Aventis Deutschland Gmbh Substituted benzoylureidopyridylpiperidine-and-pyrrolidinecarboxylic acid derivatives, processes for preparing them and their use
DE10314610A1 (de) 2003-04-01 2004-11-04 Aventis Pharma Deutschland Gmbh Neues Diphenylazetidinon mit verbesserten physiologischen Eigenschaften, Verfahren zu dessen Herstellung, diese Verbindungen enthaltende Arzneimittel und dessen Verwendung
CA2530634A1 (fr) * 2003-06-12 2004-12-23 Menachem Rubinstein Procedes permettant de traiter l'obesite et des troubles lies a l'obesite au moyen de composes contenant du tellure et du selenium
US7094800B2 (en) 2003-07-25 2006-08-22 Sanofi-Aventis Deutschland Gmbh Cyanopyrrolidides, process for their preparation and their use as medicaments
US7008957B2 (en) 2003-07-25 2006-03-07 Sanofi-Aventis Deutschland Gmbh Bicyclic cyanoheterocycles, process for their preparation and their use as medicaments
US7094794B2 (en) 2003-07-28 2006-08-22 Sanofi-Aventis Deutschland Gmbh Substituted thiazole-benzoisothiazole dioxide derivatives, process for their preparation and their use
DE10335092B3 (de) 2003-08-01 2005-02-03 Aventis Pharma Deutschland Gmbh Substituierte Benzoylureido-o-benzoylamide, Verfahren zu deren Herstellung und deren Verwendung
US7241787B2 (en) 2004-01-25 2007-07-10 Sanofi-Aventis Deutschland Gmbh Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments
US7498341B2 (en) 2004-01-31 2009-03-03 Sanofi Aventis Deutschland Gmbh Heterocyclically substituted 7-amino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments
US7470706B2 (en) 2004-01-31 2008-12-30 Sanofi-Aventis Deutschland Gmbh Cycloalkyl-substituted 7-amino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments
US7402674B2 (en) 2004-01-31 2008-07-22 Sanofi-Aventis Deutschland Gmbh, 7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments
DE102004005172A1 (de) 2004-02-02 2005-08-18 Aventis Pharma Deutschland Gmbh Indazolderivate als Inhibitoren der Hormon Sensitiven Lipase
EP1586573B1 (fr) 2004-04-01 2007-02-07 Sanofi-Aventis Deutschland GmbH Oxadiazolones, procédé pour leur préparation, usage comme agents pharmaceutiques
WO2006045799A2 (fr) 2004-10-25 2006-05-04 Solvay Pharmaceuticals Gmbh Compositions pharmaceutiques contenant des antagonistes des recepteurs cannabinoides et des agents d'ouverture de canaux potassiques dans le traitement du diabete insulino-dependant, de l'obesite et des etats associes
DE102004059470A1 (de) * 2004-12-10 2006-06-14 Lanxess Deutschland Gmbh Verfahren zur Herstellung von Carbaminsäureester-Derivaten
US20090082435A1 (en) * 2005-04-28 2009-03-26 The Regents Of The University Of California Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders
DE102005026762A1 (de) 2005-06-09 2006-12-21 Sanofi-Aventis Deutschland Gmbh Azolopyridin-2-on-derivate als Inhibitoren von Lipasen und Phospholipasen
US7737146B2 (en) 2005-10-25 2010-06-15 Council Of Scientific And Industrial Research Compound, useful for pancreatic lipase inhibition and the process for isolation thereof
AU2007225088B2 (en) 2006-03-13 2012-09-13 Kyorin Pharmaceutical Co., Ltd Aminoquinolones as GSK-3 inhibitors
DE102006028862A1 (de) 2006-06-23 2007-12-27 Merck Patent Gmbh 3-Amino-imidazo[1,2-a]pyridinderivate
BRPI0715160A2 (pt) 2006-08-08 2013-06-11 Sanofi Aventis imidazolidina-2,4-dionas substituÍdas por arilamimoaril-alquil-, processo para preparÁ-las, medicamentos compeendendo estes compostos, e seu uso
KR20090047546A (ko) 2006-09-07 2009-05-12 니코메드 게엠베하 당뇨병을 위한 조합 치료
DE102007002260A1 (de) 2007-01-16 2008-07-31 Sanofi-Aventis Verwendung von substituierten Pyranonsäurederivaten zur Herstellung von Medikamenten zur Behandlung des Metabolischen Syndroms
DE102007008420A1 (de) 2007-02-21 2008-08-28 Merck Patent Gmbh Benzimidazolderivate
US8604245B2 (en) 2007-06-04 2013-12-10 Ben-Gurion University Of The Negev Research And Development Authority Tri-aryl compounds and compositions comprising the same
CA2699151A1 (fr) 2007-09-11 2009-03-19 Activx Biosciences, Inc. Cyanoaminoquinolones et tetrazoloaminoquinolones en tant qu'inhibiteurs de gsk-3
CA2699152C (fr) 2007-09-12 2015-11-24 Activx Biosciences, Inc. Aminoquinolones spirocycliques utilisees en tant qu'inhibiteurs de gsk-3
DE102007048716A1 (de) 2007-10-11 2009-04-23 Merck Patent Gmbh Imidazo[1,2-a]pyrimidinderivate
DE102007054497B3 (de) 2007-11-13 2009-07-23 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung
DE102008017590A1 (de) 2008-04-07 2009-10-08 Merck Patent Gmbh Glucopyranosidderivate
UY31968A (es) 2008-07-09 2010-01-29 Sanofi Aventis Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos
WO2010068601A1 (fr) 2008-12-08 2010-06-17 Sanofi-Aventis Hydrate de fluoroglycoside hétéroaromatique cristallin, ses procédés de fabrication, ses procédés d'utilisation et compositions pharmaceutiques le contenant
JP2010254623A (ja) * 2009-04-24 2010-11-11 Takeda Chem Ind Ltd ベンゾオキサジノン化合物の結晶
US8785608B2 (en) 2009-08-26 2014-07-22 Sanofi Crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use
MX2012003400A (es) 2009-10-02 2012-04-10 Sanofi Sa Uso de compuestos con actividad inhibidora de sglt - 1/sglt - 2 para producir medicamentos para el tratamiento de enfermedades oseas.
AP3807A (en) * 2011-01-13 2016-09-30 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
WO2012120052A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés d'oxathiazine substitués par des carbocycles ou des hétérocycles, leur procédé de préparation, médicaments contenant ces composés et leur utilisation
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
EP2683705B1 (fr) 2011-03-08 2015-04-22 Sanofi Dérivés oxathiazine di- et tri-substitués, procédé pour leur préparation, utilisation en tant que médicament, agent pharmaceutique contenant ces dérivés et utilisation
WO2012120058A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés d'oxathiazine substitués par des groupes benzyle ou hétérométhylène, leur procédé de production, leur utilisation comme médicament ainsi que produits pharmaceutiques les contenant et leur utilisation
US8895547B2 (en) 2011-03-08 2014-11-25 Sanofi Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof
WO2012120055A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés oxathiazine di- et tri-substitués, procédé pour leur préparation, utilisation en tant que médicament, agent pharmaceutique contenant ces dérivés et utilisation
US8809324B2 (en) 2011-03-08 2014-08-19 Sanofi Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof
WO2012120053A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés oxathiazine ramifiés, procédé pour leur préparation, utilisation en tant que médicament, agents pharmaceutiques contenant ces dérivés et leur utilisation
EP2683698B1 (fr) 2011-03-08 2017-10-04 Sanofi Dérivés benzyl-oxathiazine substitués avec adamantane ou noradamantane, médicaments contenant ces composés et leur utilisation
EP2567959B1 (fr) 2011-09-12 2014-04-16 Sanofi Dérivés d'amide d'acide 6-(4-hydroxy-phényl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylique en tant qu'inhibiteurs de kinase
CA2928725A1 (fr) 2013-11-05 2015-05-14 Esther Priel Composes pour le traitement du diabete et des complications pathologiques qui en resultent
CN104374836A (zh) * 2014-09-19 2015-02-25 安徽安科生物工程(集团)股份有限公司 西替利司他及有关杂质的hplc测定方法
CN105622539B (zh) * 2016-03-11 2016-11-23 中山万汉医药科技有限公司 一种西替利司他的制备方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3450700A (en) * 1966-12-20 1969-06-17 Upjohn Co 2-tertiary amino-4h-3,1-benzoxazin-4-ones
DE2315303A1 (de) * 1973-03-27 1974-10-17 Bayer Ag Verfahren zur herstellung von n-substituierten 2-amino-3,1-benzoxazin-4-onen
US4657893A (en) * 1984-05-09 1987-04-14 Syntex (U.S.A.) Inc. 4H-3,1-benzoxazin-4-ones and related compounds and use as enzyme inhibitors
NZ210669A (en) * 1983-12-27 1988-05-30 Syntex Inc Benzoxazin-4-one derivatives and pharmaceutical compositions
US4665070A (en) 1985-06-25 1987-05-12 Syntex (U.S.A.) Inc. 2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use
US4745116A (en) 1985-06-25 1988-05-17 Syntex (U.S.A.) Inc. 2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use
US5652237A (en) * 1994-09-09 1997-07-29 Warner-Lambert Company 2-substituted-4H-3, 1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease for the treatment of inflammatory processes
US5985872A (en) * 1995-05-24 1999-11-16 G.D. Searle & Co. 2-amino-benzoxazinones for the treatment of viral infections
US5776756A (en) * 1995-08-31 1998-07-07 Toyo Hakko Co., Ltd. Fermentation compositions having superoxide dismutating activity and an antihypertensive agent for treatment of constipation each having the superoxide dismutating activity
GB9900416D0 (en) * 1999-01-08 1999-02-24 Alizyme Therapeutics Ltd Inhibitors

Also Published As

Publication number Publication date
MY129247A (en) 2007-03-30
RU2244711C2 (ru) 2005-01-20
WO2000040569A1 (fr) 2000-07-13
NO20013380D0 (no) 2001-07-06
JP2002534419A (ja) 2002-10-15
GB9900416D0 (en) 1999-02-24
US7776853B2 (en) 2010-08-17
AU770342B2 (en) 2004-02-19
PT1144395E (pt) 2005-08-31
DE60019556D1 (de) 2005-05-25
HUP0104909A2 (hu) 2002-04-29
AU1884500A (en) 2000-07-24
DK1144395T3 (da) 2005-08-15
US20030013707A1 (en) 2003-01-16
EP1144395A1 (fr) 2001-10-17
US6656934B2 (en) 2003-12-02
ES2240051T3 (es) 2005-10-16
HK1047284A1 (en) 2003-02-14
CA2359987A1 (fr) 2000-07-13
CN1354747A (zh) 2002-06-19
NO321058B1 (no) 2006-03-06
KR20010108073A (ko) 2001-12-07
KR100615914B1 (ko) 2006-08-28
WO2000040569A9 (fr) 2002-02-28
EP1144395B1 (fr) 2005-04-20
PL350412A1 (en) 2002-12-02
CA2359987C (fr) 2008-03-25
HUP0104909A3 (en) 2004-11-29
NZ512739A (en) 2003-10-31
US20030191123A1 (en) 2003-10-09
NO20013380L (no) 2001-09-07
AR022203A1 (es) 2002-09-04
DE60019556T2 (de) 2006-02-23
ATE293610T1 (de) 2005-05-15
CN100480245C (zh) 2009-04-22

Similar Documents

Publication Publication Date Title
WO2000040569A8 (fr) 2-oxy-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite
WO2000040247A8 (fr) 2-amino-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite
TW369535B (en) A pyrazolopyridine compound and the process for preparing thereof
EP1090908A3 (fr) Derives de cyclobutane utilisés comme inhibiteurs de la protéine farnesyltransferase
NZ511673A (en) Carboxylic acids and carboxylic acid isosteres of N- heterocyclic compounds
PT870765E (pt) Derivados de aminotiazole drogas contendo os mesmos e intermediarios na producao dos compostos
ES2189357T3 (es) Compustos isocromano y procedimiento para su produccion.
ES474288A1 (es) Un procedimiento para la preparacion de derivados del acido 7-oxo-1-aza-biciclo-(3,2,0)-hept-2-en-carboxilico 3 y 6-sus-tituidos
AU7517400A (en) N-substituted 4-aminopteridines, synthesis and use thereof as pharmaceutical agent
AU2001225380A1 (en) 2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors
AU2152899A (en) Pyranones, method for the production and use thereof
AU2603697A (en) Thiadiazolyl(thio)ureas useful as matrix metalloprotease inhibitors
MX9800704A (es) Esteres y amidas como inhibidores de fosfolipasa a2.
NO20010559L (no) Fremgangsmate for syntese av (1H)-benzo[c]kinolizin-3-ones derivater
AU6731100A (en) Integrase inhibitors containing aromatic heterocycle derivatives
HK1016591A1 (en) Pyrimidine derivatives
MXPA04000485A (es) Uso de acidos aril o heteroaril hidroxamicos de sulfonilo y derivados de los mismos como inhibidores de agrecanasa.
IL151167A0 (en) Pyrrolopyridazine derivatives and pharmaceutical compositions containing the same
WO2003015781A1 (fr) Nouvelles compositions pharmaceutiques antidiabetiques
TW200502204A (en) Oligo acid derivatives
MY139608A (en) Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity
AU5114993A (en) Method for the stereoselective preparation of a derivative of beta -phenylisoserine and its use in the preparation of taxane derivatives
Adam et al. Potential prodrugs of 6-acetylmethylenepenicillanic acid (Ro 15-1903)
TH59783B (th) ตัวยับยั้ง
PT868428E (pt) Derivados de acido fosfonico possuindo actividade inibidora da metalopeptidase

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 00803621.7

Country of ref document: CN

AK Designated states

Kind code of ref document: A1

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
AK Designated states

Kind code of ref document: C1

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: C1

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

WR Later publication of a revised version of an international search report
AK Designated states

Kind code of ref document: B8

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: B8

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

CFP Corrected version of a pamphlet front page
CR1 Correction of entry in section i
WWE Wipo information: entry into national phase

Ref document number: 512739

Country of ref document: NZ

WWE Wipo information: entry into national phase

Ref document number: 18845/00

Country of ref document: AU

ENP Entry into the national phase

Ref document number: 2359987

Country of ref document: CA

Ref document number: 2359987

Country of ref document: CA

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 09901868

Country of ref document: US

Ref document number: 1020017008596

Country of ref document: KR

Ref document number: PA/a/2001/006920

Country of ref document: MX

ENP Entry into the national phase

Ref document number: 2000 592277

Country of ref document: JP

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 2000900081

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 2000900081

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: 1020017008596

Country of ref document: KR

AK Designated states

Kind code of ref document: C2

Designated state(s): AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZW

AL Designated countries for regional patents

Kind code of ref document: C2

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

COP Corrected version of pamphlet

Free format text: PAGES 1-54, DESCRIPTION, REPLACED BY CORRECT PAGES 1-51; PAGES 55-67, CLAIMS, REPLACED BY CORRECT PAGES 52-63

WWG Wipo information: grant in national office

Ref document number: 18845/00

Country of ref document: AU

WWG Wipo information: grant in national office

Ref document number: 2000900081

Country of ref document: EP

WWG Wipo information: grant in national office

Ref document number: 1020017008596

Country of ref document: KR

DPE2 Request for preliminary examination filed before expiration of 19th month from priority date (pct application filed from 20040101)